SB-743921 hydrochloride

SKU: orb1305882

Description

SB-743921 hydrochloride is a potent and selective inhibitor of kinesin spindle protein (KSP) with a Ki of 0.1 nM. It induces mitotic arrest and has demonstrated antitumor activity in both cellular assays and in vivo xenograft models, making it a valuable tool for cancer research.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 940929-33-9
• MW: 553.52
• Purity: 99.70% (May vary between batches)
• Formula: C₃₁H₃₄Cl₂N₂O₃
• SMILES: Cl.CC(C)[C@@H](N(CCCN)C(=O)c1ccc(C)cc1)c1oc2cc(Cl)ccc2c(=O)c1Cc1ccccc1
• Target: KSP,Kinesin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.61 mM);DMSO:60 mg/mL (108.4 mM)

Bioactivity

• Target IC50:
  KSP:0.1 nM(Ki)
• In Vivo:
  SB 743921 inhibits the formation of the mitotic spindle, thereby accumulating cells in mitosis and inducing cell necrosis. It is effective against human KSP (Ki=0.1 nM) and mouse KSP (Ki=0.12 nM).
• In Vitro:
  The chemical compound exhibits a notable inhibitory effect on the growth of a wide range of heterograft tumors in humans, such as Colo205, MCF-7, SK-MES-1, H69, OVCAR-3, HT-29, MX-1, MDA-MB-231, A2780, and SB-743921, effectively suppressing cellular proliferation.
• Cell Research:
  All cells including HeLa cells are cultured in 10% FCS in RPMI 1640 in 5% CO2. We assessed 48-hour growth inhibition by serial dilution of SB 743921 relative to DMSO-treated cells in 96-well microtiter plates, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium. Cell growth is represented as the ratio of absorbance of treated cells to DMSO control, plotted by concentration and fitted to a four-parameter curve. Concentrations at which cellular growth is inhibited by 50% are extrapolated from the curve fit. The DNA content of HeLa cells cultured in the presence or absence of 1 μM SB 743921 for 24 hours is assessed by propidium iodide staining and flow cytometry. Immunofluorescence images are collected of HeLa cells treated for 24 hours with 1 μM SB 743921, fixed with 2% formaldehyde, permeabilized, and stained with DM1-α, anti-γ-tubulin, and 1 μg/mL 4′,6-diamidino-2-phenylindole, and with Alexa 488 secondary goat antirabbit IgG and Rhodamine-X goat antimouse IgG. Images are collected with a DeltaVision Restoration Microscopy System at a magnification of ×600. Z stacks (0.2 μm) are collected, and out of focus information is removed by constrained iterative deconvolution. Z stacks are then compressed into to a single image plane. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB743921 HCl, SB-743921 Hydrochloride, KSP, KSP (Colo205 cells), KSP (MV522 cells), KSP (MX1 cells), KSP (SKOV3 cells), Kinesin

Compound Identifiers

PubChem CID

49867937